Investigational New Drugs

, Volume 30, Issue 5, pp 1899–1907 | Cite as

ZJU-6, a novel derivative of Erianin, shows potent anti-tubulin polymerisation and anti-angiogenic activities

  • Frankie Lam
  • Tracey D. Bradshaw
  • Hui Mao
  • Scott Roberts
  • Yuanjiang Pan
  • Shudong Wang


ZJU-6 was designed to enhance anti-angiogenesis and anti-tumour activity of its parent compound Erianin, a clinic anti-tumour agent. This study investigated the detailed biological mechanism of ZJU-6 in comparison with that of Erianin. Both ZJU-6 and Erianin substantially reduced cell viability and induced apoptosis in human cancer cell lines. Profound G2/M cell arrest was observed 24 h after treatment of MCF-7 cells with ZJU-6 (≥ 2.5 μM) or Erianin (≥ 0.1 μM); being consistent with mitotic collapse. 0.5 μM of Erianin or ZJU-6 failed to stabilise tubulin. Pre-G1 MCF-7 cell accumulating 24 h post treatment indicated apoptosis. Caspase-3 activity, PARP cleavage and Annexin V + ve /PI -ve populations correlate the apoptotic destiny of cells exposed to either ZJU-6 or Erianin. Furthermore ZJU-6 showed potent anti-angiogenetic property and demonstrated radical scavenging capacity. Due to its potent anti-proliferative, pro-apoptotic and anti-angiogenic activities ZJU-6 is an attractive chemotherapeutic agent to be developed.


Apoptosis Anti-tubulin polymerisation Caspase activation Angiogenesis Anti-oxidant Chemotherapy 



This work has been supported by The Royal Society, UK (grant RC2617) and NSFC, China

Conflicts of interest

No potential conflicts of interest are disclosed.


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Copyright information

© Springer Science+Business Media, LLC 2011

Authors and Affiliations

  • Frankie Lam
    • 1
  • Tracey D. Bradshaw
    • 1
  • Hui Mao
    • 2
  • Scott Roberts
    • 1
  • Yuanjiang Pan
    • 2
  • Shudong Wang
    • 1
  1. 1.School of Pharmacy and Centre for Biomolecular SciencesUniversity of NottinghamNottinghamUK
  2. 2.Department of ChemistryZhejiang UniversityHangzhouPeople’s Republic of China

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